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Dissociation Constant I: Agonists

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Abstract

An agonist and an antagonist that act on the same receptor are used in this determination. The antagonist must bind irreversibly to the receptor; its presence, therefore, inactivates the receptors to which it combines. If the antagonist concentration is not too great, it will inactivate only a fraction of the total receptor pool and produce a depression of the agonist’s dose—response curve. These curves are shown in Figure 12.1, curve (1) for the agonist alone and curve (2) for the agonist in the presence of the antagonist.

Furchgott, R.F., and Bursztyn, P. Ann. N.Y. Acad. Sci. 144:882, 1967.

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© 1987 Springer-Verlag New York Inc.

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Tallarida, R.J., Murray, R.B. (1987). Dissociation Constant I: Agonists. In: Manual of Pharmacologic Calculations. Springer, New York, NY. https://doi.org/10.1007/978-1-4612-4974-0_13

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  • DOI: https://doi.org/10.1007/978-1-4612-4974-0_13

  • Publisher Name: Springer, New York, NY

  • Print ISBN: 978-1-4612-9380-4

  • Online ISBN: 978-1-4612-4974-0

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